| 产品描述： | Adezmapimod (SB 203580) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride is an autophagy and mitophagy activator |
| 靶点： |
p38:50 nM (IC50);p38β2:500 nM (IC50) |
| 体外研究： |
Adezmapimod hydrochloride (用 0-30 μM 预孵育 1 小时并在 20 ng/mL IL-2 存在下培养 24 小时) 可防止 IL-2 诱导的原代人 T 细胞、鼠 CT6 T 细胞或 BAF 增殖 F7 B 细胞的 IC50 为 3-5 μM。 Adezmapimod hydrochloride 阻断 PKB 磷酸化 (IC50 3-5 μM)。Adezmapimod hydrochloride 在 CT6 和活化的人 T 细胞以及 IL-2 反应性 BA/F3 F7 B 细胞中以剂量依赖性方式抑制 Ser473 的磷酸化。 Cell Proliferation Assay Cell Line: CT6, BA/F3 cell line F7, and PBMC/T cells Concentration: 0-30 μM Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h and cultured for 24 h in the presence of 20 ng/mL IL-2 Result: Prevented the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3-5 μM. Western Blot Analysis Cell Line: CT6 cells, activated human T cells, and BA/F3 F7 cells Concentration: 0-30 μM Incubation Time: Preincubated with 0-30 μM SB203580 for 1 h before stimulating with 20 ng/mL IL-2 for 5 min Result: Inhibited the phosphorylation of PKB at Ser473 in a dose-dependent manner. |
| 体内研究： |
Adezmapimod hydrochloride (5 mg/kg/day； 连续16天每天腹膜内注射； 雌性无胸腺 Nu/Nu 小鼠) 处理与平行处理的 p38TM 肿瘤相比，p38WT 肿瘤的肿瘤负荷明显更小。 Animal Model: Six-week-old female atymic Nu/Nu mice CAL27 p38WT and p38TM tumors Dosage: 5 mg/kg/day Administration: Intra peritoneal injected daily for 16 consecutive days Result: After 2 weeks treatment, CAL27 p38WT tumors were significantly smaller; CAL27 p38TM tumors were not affected by the p38 inhibitor (n=10). |
| 参考文献： |
1. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. 2. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402. 3. Leelahavanichkul K, et al. A role for p38 MAPK in head and neck cancer cell growth and tumor-induced angiogenesis and lymphangiogenesis. Mol Oncol. 2014 Feb;8(1):105-18. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.416 ml |
12.08 ml |
24.16 ml |
| 5 mM |
0.483 ml |
2.416 ml |
4.832 ml |
| 10 mM |
0.242 ml |
1.208 ml |
2.416 ml |
| 50 mM |
0.048 ml |
0.242 ml |
0.483 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京